Application of 60811-21-4,Some common heterocyclic compound, 60811-21-4, name is 4-Bromo-2-chloro-1-fluorobenzene, molecular formula is C6H3BrClF, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
Step 1: tert-Butyl 4-(3-chloro-4-fluorophenyl)piperazine-1-carboxylate A solution of tert-butyl-piperazine-1-carboxylate (1.0 g, 5.37 mmol), 4-bromo-2-chloro-1-fluorobenzene (1.35 g, 6.44 mmol), t-BuONa (768 mg, 8.06 mmol), BINAP (125 mg, 0.2 mmol), Pd2(dba)3 (92 mg, 0.1 mmol) in dry toluene (10 mL) was stirred under N2 at 80 C. for 16 hrs. The reaction mixture was concentrated and the mixture was purified by chromatography (silica, EtOAc/PE=1/10) to afford tert-butyl-4-(3-chloro-4-fluorophenyl)piperazine-1-carboxylate (1.3 g, 4.13 mmol, 77%) as a yellow oil. ESI-MS (EI+, m/z): 259 [M-55]+.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 4-Bromo-2-chloro-1-fluorobenzene, its application will become more common.
Reference:
Patent; Navitor Pharmaceuticals, Inc.; O’Neill, David John; Saiah, Eddine; Kang, Seong Woo Anthony; Brearley, Andrew; Bentley, Jonathan; (136 pag.)US2019/389843; (2019); A1;,
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